TG003

TG003 (CAS No.: 719277-26-6) is a selective, small-molecule inhibitor of the Cdc2-like kinase (Clk) family, with potent activity against Clk1 and Clk4, key regulators of serine/arginine-rich (SR) protein phosphorylation during pre-mRNA splicing. By modulating Clk-mediated phosphorylation events, TG003 effectively alters alternative splicing patterns and downstream gene expression programs, making it a valuable chemical probe for investigating RNA splicing mechanisms and post-transcriptional regulation. The compound exhibits inhibitory activity in the nanomolar range toward its primary targets, supporting its utility in mechanistic studies of spliceosome dynamics and signal-dependent splicing control. In cellular systems, TG003 has been shown to influence proliferation and apoptosis, providing a functional tool for exploring the role of aberrant splicing in disease-relevant models, including cancer biology and neuromuscular disorders. Its application extends to studies of signaling pathways that intersect with RNA processing, as well as to compound screening efforts aimed at identifying modulators of splicing factor activity. Experimental concentrations and treatment regimens vary depending on the specific cell type, assay design, and research objectives.